一般描述
A highly specific, cell-permeable inhibitor of p38 kinase (IC50 = 34 nM in vitro, 600 nM in cells). Also known as reactivating kinase (RK) and CSBP (cytokine synthesis anti-inflammatory drug binding protein). Does not significantly inhibit JNK or p42 MAP kinase even at 100 µM. Inhibits IL-1 and TNF-α production from LPS-stimulated human monocytes and the human monocyte cell line THP-1 (IC50 = 50-100 nM). SB 203580 has also been shown to be an effective inhibitor of inflammatory cytokine production in vivo in both mice and rats.
生化/生理作用
Cell permeable: yes
Product competes with ATP.
Reversible: yes
Target IC50: 34 nM in vitro, 600 nM in cells against p38 MAPK; 50-100 nM Inhibiting IL-1 and TNF-α production from LPS-stimulated human monocytes and the human monocyte cell line THP-1; 0.2-1.0 µM inhibiting platelet aggregation by collagen
包装
Packaged under inert gas
外形
A 1 mg/ml solution of SB 203580 (Cat. No. 559389) in anhydrous DMSO.
其他说明
Powell, D.J., et al. 2003. Mol. Cell Biol.23, 7794.
Davies, S.P., et al. 2000. Biochem. J.351, 95.
Iwasaki, S., et al. 1999. J. Biol. Chem.274, 26503.
Gallagher, T.F., et al. 1997. Bioorg. Med. Chem. 5, 49.
LoGrasso, P.V., et al. 1997. Biochem. 36, 10422.
Hazzalin, C.A., et al. 1996. Curr. Biol.6, 1028.
Kramer, R.M., et al. 1996. J. Biol. Chem.271, 27723.
Saklatvala, J., et al. 1996. J. Biol. Chem. 271, 6586.
Cuenda, A., et al. 1995. FEBS Lett.364, 229.
Gallagher, T.F., et al. 1995. Bioorg. Med. Chem. Lett. 5, 1171.
Lee, J.C., et al. 1994. Nature 372, 739.
Davies, S.P., et al. 2000. Biochem. J.351, 95.
Iwasaki, S., et al. 1999. J. Biol. Chem.274, 26503.
Gallagher, T.F., et al. 1997. Bioorg. Med. Chem. 5, 49.
LoGrasso, P.V., et al. 1997. Biochem. 36, 10422.
Hazzalin, C.A., et al. 1996. Curr. Biol.6, 1028.
Kramer, R.M., et al. 1996. J. Biol. Chem.271, 27723.
Saklatvala, J., et al. 1996. J. Biol. Chem. 271, 6586.
Cuenda, A., et al. 1995. FEBS Lett.364, 229.
Gallagher, T.F., et al. 1995. Bioorg. Med. Chem. Lett. 5, 1171.
Lee, J.C., et al. 1994. Nature 372, 739.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
免责声明
Toxicity: Irritant (B)
储存分类代码
10 - Combustible liquids
WGK
WGK 2
闪点(°F)
188.6 °F - closed cup - (Dimethylsulfoxide)
闪点(°C)
87 °C - closed cup - (Dimethylsulfoxide)
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